Rubin J R, Sabat M, Sundaralingam M
Nucleic Acids Res. 1983 Sep 24;11(18):6571-86. doi: 10.1093/nar/11.18.6571.
A comparative study of the binding of square planar cis- and trans-[Pt(NH3)2Cl2] complexes and the octahedral [Ru(NH3)5(H2O)]3+ complex to tRNAphe from yeast was carried out by X-ray crystallography. Both of the carcinostatic compounds, cis-[Pt(NH3)2Cl2] and [Ru(NH3)5(H2O)]3+ show similarities in their mode of binding to tRNA. These complexes bind specifically to the N(7) positions of guanines G15 and G18 in the dihydrouridine loop. [Ru(NH3)5(H2O)]3+ has an additional binding site at N(7) of residue G1 after extensive soaking times (58 days). A noncovalent binding site for ruthenium is also observed in the deep groove of the acceptor stem helix with shorter (25 days) soaking time. The major binding site for the inactive trans-[Pt(NH3)Cl2] complex is at the N(1) position of residue A73, with minor trans-Pt binding sites at the N(7) positions of residues Gm34, G18 and G43. The similarities in the binding modes of cis-[Pt(NH3)2Cl2] and [Ru(NH3)5(H2O)]3+ are expected to be related to their carcinostatic properties.
通过X射线晶体学对平面正方形顺式和反式-[Pt(NH₃)₂Cl₂]配合物以及八面体[Ru(NH₃)₅(H₂O)]³⁺配合物与来自酵母的tRNAphe的结合进行了比较研究。两种抗癌化合物,顺式-[Pt(NH₃)₂Cl₂]和[Ru(NH₃)₅(H₂O)]³⁺在与tRNA的结合模式上显示出相似性。这些配合物特异性地结合到二氢尿嘧啶环中鸟嘌呤G15和G18的N(7)位置。经过较长浸泡时间(58天)后,[Ru(NH₃)₅(H₂O)]³⁺在残基G1的N(7)处有一个额外的结合位点。在较短浸泡时间(25天)下,在受体茎螺旋的深沟中也观察到钌的一个非共价结合位点。无活性的反式-[Pt(NH₃)Cl₂]配合物的主要结合位点在残基A73的N(1)位置,在残基Gm34、G18和G43的N(7)位置有次要的反式铂结合位点。顺式-[Pt(NH₃)₂Cl₂]和[Ru(NH₃)₅(H₂O)]³⁺结合模式的相似性预计与它们的抗癌特性有关。